JP2007537296A5 - - Google Patents

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JP2007537296A5
JP2007537296A5 JP2007513433A JP2007513433A JP2007537296A5 JP 2007537296 A5 JP2007537296 A5 JP 2007537296A5 JP 2007513433 A JP2007513433 A JP 2007513433A JP 2007513433 A JP2007513433 A JP 2007513433A JP 2007537296 A5 JP2007537296 A5 JP 2007537296A5
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Priority claimed from PCT/US2005/016903 external-priority patent/WO2005110410A2/en
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均一時間分割蛍光（ＨＴＲＦ）イン・ビトロキナーゼアッセイ（Mathis, G., HTRF(R) Technology. J Biomol Screen, 1999. 4(6): p. 309-314参照；これの内容は、参照によって本明細書に全体が組み込まれる。）
精製酵素（商業的入手源から入手可能）を、各種反応緩衝液中の各種阻害薬濃度での各種量のＮ−ビオチン処理基質もしくはＧＳＴ−標識基質（表を参照）（最終容量４０μＬ、表を参照。）と混合した。黒色９６−ハーフ−ウェルプレート（Perkin Elmer）中にてＡＴＰ（最終濃度０．０１〜０．１ｍＭ）を加えることで、キナーゼ反応を開始した。室温で５０〜６０分間インキュベーションした後、ＥＤＴＡ（最終濃度１００ｍＭ）を加えることで反応停止し、顕色試薬を加えることで現像した（大体の最終濃度：３０ｍＭ ＨＥＰＥＳ、ｐＨ７．０、０．０６％ＢＳＡ、０．００６％Ｔｗｅｅｎ−２０、０．２４μＭ ＫＦ、その酵素反応に対して特異的である各種量のドナーユーロピウム（eutropium）標識抗体および受容体ストレプトアビジン標識アロフィコシアニン（ＳＡＸＬ）またはＧＳＴ−ＸＬ；表参照。）。現像した反応液を、暗所にて室温で１０分間または４℃で終夜インキュベートし（表参照）、時間分割蛍光検出器で６２０ｎｍおよび６６５ｎｍにて同時に読み取った（ディスカバリー（Discovery）、パーキン・エルマー（Perkin Elmer）もしくはルビースター（Rubystar）、ＢＭＧ）。３３７ｎｍ窒素レーザーを励起に用いた。６２０ｎｍと６６５ｎｍとの間のシグナルの比を用いて、ＩＣ５０を計算した。
Figure 2007537296
Figure 2007537296
Figure 2007537296
JP2007513433A 2004-05-14 2005-05-13 治療薬としてのキナーゼ阻害薬 Withdrawn JP2007537296A (ja)

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US57128104P 2004-05-14 2004-05-14
PCT/US2005/016903 WO2005110410A2 (en) 2004-05-14 2005-05-13 Kinase inhibitors as therapeutic agents

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JP2007537296A JP2007537296A (ja) 2007-12-20
JP2007537296A5 true JP2007537296A5 (ja) 2008-03-06

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US (1) US20060074102A1 (ja)
EP (1) EP1753428A4 (ja)
JP (1) JP2007537296A (ja)
CA (1) CA2566158A1 (ja)
MX (1) MXPA06013250A (ja)
WO (1) WO2005110410A2 (ja)

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